Abstract: A method and means for delivery of drugs to the chorio-retina and the optic nerve head which comprises contacting the surface of the eye with an effective amount of drug for treatment of chorio-retina and optic nerve head and a physiologically acceptable adrenergic agent for enhancing delivery of the drug to these tissues in an ophtalmologically acceptable carrier, said adrenergic agent being selected from the group consisting of alpha adrenergic agonist agents, derivatives of the alpha adrenergic agonist agents, beta-blocking agents, derivatives of the beta-blocking agents and mixtures thereof.

Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.

Abstract: The invention relates to a topical composition and a method for treating psoriasis. The topical composition comprises one or more compound that inhibits the production of IL-12 and IL-23.

Abstract: The present invention provides a process for preparing optically active timolol. The process comprises the following steps. Firstly, reacting 3-hydroxy-4-morpholino-1,2,5-thiadiazole with an optically active epichlorohydrin in the presence of a solvent system, which has a first volume and a catalyst optionally in the presence of a suitable base to obtain an optically active intermediate product. Secondly, treating the optically active intermediate product with a solution, which has a second volume and comprises tert-butylamine to obtain an optically active timolol. The solvent system used in the first step can be an amide solvent, sulfoxide solvent, cyclic hydrocarbon solvent, ketone solvent, or a heterocyclic solvent. The catalyst used in the first step can be an alkali metal hydroxide, alkali metal carbonate, alkali metal hydrogen carbonate, piperidine, pyridine, triethylamine, potassium hydroxide, sodium hydroxide, potassium carbonate, and other heterocyclic bases.

Abstract: Biocompatible intraocular implants include a beta adrenergic receptor antagonist and a polymer associated with the beta adrenergic receptor antagonist to facilitate release of the beta adrenergic receptor antagonist into an eye for an extended period of time. The beta adrenergic receptor antagonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat one or more ocular conditions, such as an ocular neuropathies, for example, various forms of glaucoma.

Abstract: The present invention relates to new thiadiazole modulators of beta adrenergic receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Methods of using triazole derivatives in treating diseases or conditions associated with Axl catalytic activity are disclosed.

Abstract: 1,2,4-Triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I), pharmaceutically acceptable salts thereof, processes for the manufacture of 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives and pharmaceutical compositions containing 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives are disclosed: The 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I) possess cell cycle inhibitory activity and are accordingly useful for their anti cell proliferation (such as anti cancer) activity.

Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.

Abstract: Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110? isoform of PI3K.

Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3 and R4 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: The present invention relates to compounds for treating or preventing infection that inhibit the activity of Hsp90.

Abstract: The present disclosure provides methods and compositions for treating Impulse Control disorders including, for example, pathological gambling using ?2-adrenergic agonists, ?-adrenergic receptor antagonists, or both.

Abstract: The present invention relates to functional proteins encoded by nucleic acid sequences comprising a nonsense mutation. The present invention also relates to methods for the production of functional proteins encoded by nucleic acid sequences comprising a nonsense mutation and the use of such proteins for prevention, management and/or treatment of diseases associated with a nonsense mutation(s) in a gene.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: Disclosed herein are stable formulations suitable for the treatment of glaucoma and ocular hypertension.

Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.

Abstract: A method for treating diabetic complications by administration of a beta-blocker is disclosed. Diabetic complications arise from diabetes and have few or no existing treatment options. The present invention describes the use of a beta-blocker in the treatment of a diabetic. The present invention also describes the inhibition of aldose reductase, one of the chief causative factors of diabetic complications. Also provided are methods of diabetic wound healing. Compositions for treating diabetic complications, such as diabetic wounds, are disclosed. The present invention includes employing a topical formulation of a beta-blocker, having substantially no antibacterial activity, to improve the process of diabetic wound healing. The present invention also involves increasing the rate of collagen accumulation of the healing epithelialized tissue in the wound of a diabetic individual.

Abstract: The present invention provides compounds of Formula (I): in which R1, R?1, R2, R?2, R3, and Y have the meanings given in the description are useful in the treatment of conditions susceptible to modulating ion channels, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: Solubility-enhanced forms of aprepitant and processes for preparing such forms. The invention also provides solubility-enhanced forms of aprepitant that also possess stability against solid state conversions. Certain solubility-enhanced forms of aprepitant comprise a cyclodextrin or any of its derivatives. Other solubility-enhanced forms of aprepitant comprise fine particle preparations of aprepitant. The invention further provides non-nanoparticulate pharmaceutical formulations prepared using solubility-enhanced forms of aprepitant. The invention also provides taste-masked and orally disintegrating pharmaceutical formulations comprising aprepitant. Further, pharmaceutical formulations comprising solubilityenhanced forms of aprepitant and processes of preparation of such formulations, as well as methods of using them are provided.

Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: The present invention relates to compounds of Formula (I): where in X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: An ophthalmic composition comprising therapeutically effective amount of a beta-blocker and a polymeric vehicle consisting essentially of a water soluble cellulose derivative and polyvinylpyrrolidone; wherein the composition is a clear aqueous solution with a viscosity id 20 cps to 60 cps.

Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.

Abstract: The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract: An appliance for the delivery of at least one bioactive agent to the eye has at least one diffusion attenuator within a hydrophilic or silicone-hydrogel contact lens. The bioactive agent can be a drug or a nutraceutical. The diffusion attenuator can be a plurality of solid particles or phase separated liquid aggregates within at least one continuous phase of the lens where the diffusion attenuators promote a tortuous path for the diffusion of the bioactive agent to mediate the rate by which the bioactive agent diffuses from the contact lens. The diffusion attenuator can be homogeneously dispersed throughout at least one continuous phase of the lens to modify the diffusivity of the bioactive agent through that phase. The diffusion attenuator can have little or no affinity for the bioactive agent or can be miscible with the bioactive agent. The diffusion attenuator can be incorporated while forming the contact lens by polymerization of a monomer mixture containing the diffusion attenuator.

Abstract: The present invention relates to the CGRP antagonists of general formula I wherein R1, R2, R3 and R4 are as defined in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: Compounds of formula (I), and salts and pro-drugs thereof: wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.

Abstract: The present invention relates generally to the field of pain management, and in particular, the management of neuropathic pain. The present invention further provides methods and compositions that treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic pain without inducing overt sedation. The present invention also contemplates combination therapy using one or more NK antagonists in combination with one or more compounds which decrease or inhibit neuronal excitation in the treatment of pain in association with the treatment of a particular disease condition or pathology.

Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable derivatives thereof wherein the variables Z, Q, Ring A, V, X, Y and Y? are as defined herein, and pharmaceutical compositions comprising these compounds. The compounds of formula (I) and pharmaceutical compositions comprising them are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.

Abstract: Methods and compounds are disclosed for affecting gastrointestinal motility and gastric emptying, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof

Abstract: A punctal plug and method of treating dry eyes are provided. The punctal plug has two or three layer structure and contains at least one drug, for treating conditions such as dry eyes contained in a core, a potion of which is covered by a drug impermeable shell such that drug can radially diffuse from the core. The punctal plug can be inserted into a patient's upper punctum, lower punctum, or both to deliver the drug for an extended period of time. The drug for treating dry eyes can be, for example, cyclosporine A. The plug can also be used for extended delivery of ophthalmic drugs.

Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

Abstract: The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.

Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.

Abstract: Intimate mixtures of aprepitant crystalline Form I and crystalline Form II, having specific Hweight ratios of the forms.

Abstract: The present invention relates to substituted triazole compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming A?42 peptide such as Alzheimer's disease and the like.

Abstract: This invention relates to novel benzamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.

Abstract: A pyridine compound represented by the following general formula (1); the pyridine compound in which R1 is a C1-C3 fluoroalkyl group or a C1-C3 fluoroalkoxy group; the pyridine compound in which R2 is a hydrogen atom; the pyridine compound in which R2 is a group represented by Q; a pesticidal composition containing the pyridine compound as an active ingredient; and a method of controlling a pest including applying an effective amount of the pyridine compound to the pest or a place where the pest inhabits, are provided.

Abstract: The invention provides a pharmaceutical combination comprising: a) at least one agent selected from Bcr-Abl, Flt-3, FAK and RAF kinase inhibitors; and b) at least one JAK kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.

Abstract: The present invention relates to a method for suppressing the immune system in a subject in need thereof, and a method for treating an inflammatory or immune disorder in a subject in need thereof.

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.

Abstract: The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or 2 or encompassed by formula I) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.